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1.
Medicina (Kaunas) ; 59(10)2023 Oct 12.
Artículo en Inglés | MEDLINE | ID: mdl-37893532

RESUMEN

Background and Objectives: Paracetamol overdose is a significant global issue due to its widespread use, which can lead to a lack of awareness regarding its potential side effects. Paracetamol can harm the liver, possibly resulting in liver failure. Conversely, this study employed extracts from Petroselinum crispum (PC), known for its rich content of bioactive compounds, with demonstrated antioxidant properties shown in previous research as well as protective effects against various diseases. The primary objective of this study was to investigate the potential protective effects of Petroselinum crispum on altered hematological and biochemical parameters in the blood of rats exposed to paracetamol. Materials and Methods: The study involved twenty Wistar rats divided into four groups. Different groups of male rats were administered PC extract at 200 mg/kg body weight daily for 15 days, along with a standard reference dose of paracetamol at 200 mg/kg. The study assessed hepatoprotection capacity by analyzing liver enzymes such as aspartate aminotransferase (AST), alanine aminotransferase (ALT), bilirubin, albumin, and lipid profiles. Renal safety was evaluated through creatinine, urea, uric acid, lactate dehydrogenase (LDH), and total protein. Additionally, histopathological examinations of the liver and kidneys were conducted. Results: Following Paracetamol overdose, there were reductions in hemoglobin levels, serum total protein, albumin, and uric acid. Paracetamol overdose also elevated levels of several blood biomarkers, including creatinine, urea, nitrogen, ALT, AST, triglycerides, LDH activity, white blood cell count, and platelet count compared to the control group. However, using an ethanolic extract of Petroselinum crispum significantly mitigated the severity of these alterations and the extent of the effect correlated with the dose administered. Parsley extract helped prevent proteinuria and low hemoglobin, which are common side effects of Paracetamol. Conclusions: Therefore, parsley may hold promise in managing liver and kidney conditions-particularly in addressing proteinuria. Ultimately, these results may have implications for human health by potentially mitigating paracetamol-induced renal, hepatic, and hematological toxicity.


Asunto(s)
Acetaminofén , Efectos Colaterales y Reacciones Adversas Relacionados con Medicamentos , Humanos , Ratas , Masculino , Animales , Acetaminofén/toxicidad , Petroselinum , Ratas Wistar , Ácido Úrico/farmacología , Creatinina/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Extractos Vegetales/metabolismo , Hígado , Proteinuria , Albúminas , Urea , Hemoglobinas
2.
Molecules ; 29(1)2023 Dec 22.
Artículo en Inglés | MEDLINE | ID: mdl-38202676

RESUMEN

Cannabis is considered (Cannabis sativa L.) a sacred herb in many countries and is vastly employed in traditional medicine to remedy numerous diseases, such as diabetes. This research investigates the chemical composition of the aqueous extracts from Cannabis sativa L. seeds. Furthermore, the impact of these extracts on pancreatic α-amylase and lipase, and intestinal α-glucosidase enzymes is evaluated, as well as their antihyperglycemic effect. Analysis of the chemical composition of the aqueous extract was conducted using high-performance liquid chromatography with a photodiode array detector (HPLC-DAD). In contrast, the ethanol, hexanic, dichloromethane, and aqueous extract compositions have been established. Additionally, the inhibitory effects of ethanolic, dichloromethane, and aqueous extracts on pancreatic α-amylase and lipase, and intestinal α-glucosidase activities were evaluated in vitro and in vivo. The results of HPLC analysis indicate that the most abundant phenolic compound in the aqueous cannabis seed extract is 3-hydroxycinnamic acid, followed by 4-hydroxybenzoic acid and rutin acid. Moreover, administration of ethanolic and aqueous extracts at a dose of 150 mg/Kg significantly suppressed postprandial hyperglycemia compared to the control group; the ethanolic, dichloromethane, and aqueous extracts significantly inhibit pancreatic α-amylase and lipase, and intestinal α-glucosidase in vitro. The pancreatic α-amylase test exhibited an inhibition with IC50 values of 16.36 ± 1.24 µg/mL, 19.33 ± 1.40 µg/mL, 23.53 ± 1.70 µg/mL, and 17.06 ± 9.91 µg/mL for EAq, EDm, EET, and EHx, respectively. EET has the highest inhibitory capacity for intestinal α-glucosidase activity, with an IC50 of 32.23 ± 3.26 µg/mL. The extracts inhibit porcine pancreatic lipase activity, demonstrating their potential as lipase inhibitors. Specifically, at a concentration of 1 mg/mL, the highest inhibition rate (77%) was observed for EDm. To confirm these results, the inhibitory effect of these extracts on enzymes was tested in vivo. The oral intake of aqueous extract markedly reduced starch- and sucrose-induced hyperglycemia in healthy rats. Administration of the ethanolic extract at a specific dose of 150 mg/kg significantly reduced postprandial glycemia compared with the control group. It is, therefore, undeniable that cannabis extracts represent a promising option as a potentially effective treatment for type 2 diabetes.


Asunto(s)
Cannabis , Diabetes Mellitus Tipo 2 , Alucinógenos , Hiperglucemia , Animales , Ratas , Porcinos , Hipoglucemiantes/farmacología , alfa-Amilasas Pancreáticas , alfa-Glucosidasas , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Cloruro de Metileno , Lipasa , Hiperglucemia/tratamiento farmacológico , Agonistas de Receptores de Cannabinoides , Etanol , Extractos Vegetales/farmacología
3.
Artículo en Inglés | MEDLINE | ID: mdl-35815261

RESUMEN

The goal of the current study was to assess the nephroprotective and cardioprotective potential of Moricandia sinaica methanol extract (MOR-1), as well as its butanol (MOR-2) and aqueous (MOR-3) fractions against carbon tetrachloride (CCl4)-induced nephro and cardio-toxicity. Cardiac function was assessed using the biochemical parameters lactate dehydrogenase (LDH) and creatinine kinase (CK). Renal function was examined using the biochemical parameters creatinine and uric acid. The levels of nonprotein sulfhydryls (NPSH) and malondialdehyde (MDA) were used as markers of oxidative strain. A dose of 100 and 200 mg/kg of butanol fraction given prior to CCl4 treatment significantly (p < 0.05 - 0.001) protected against elevated LDH and CK levels. Similarly, treatment with silymarin (10 mg/kg) and butanol fraction (100 and 200 mg/kg) significantly (p < 0.05 - 0.001) boosted total protein levels compared to CCl4 treatment alone. The silymarin (10 mg/kg) and butanol fraction (100 and 200 mg/kg) also provided a significant (p < 0.05 - 0.001) protective effect for MDA levels. Methanol extract (MOR-1) and butanol (MOR-2) showed significant results and were recommended for further pharmacological and screening for active constituents.

4.
Artículo en Inglés | MEDLINE | ID: mdl-35463088

RESUMEN

Mentha spicata, also called Mentha viridis, is a medicinal plant of the Lamiaceae family characterized by its potency to synthesize and secret secondary metabolites, essentially essential oils. Different populations use the aerial parts of this plant for tea preparation, and this tisane has shown several effects, according to ethnopharmacological surveys carried out in different areas around the world. These effects are attributed to different compounds of M. spicata, in which their biological effects were recently proved experimentally. Pharmacological properties of M. spicata extracts and essential oils were investigated for different health benefits such as antioxidant, anticancer, antiparasitic, antimicrobial, and antidiabetic effects. In vitro and in vivo studies showed positives effects that could be certainly related to different bioactive compounds identified in M. spicata. Indeed, volatile compounds seem to be efficient in inhibiting different microbial agents such as bacteria, fungi, and parasites through several mechanisms. Moreover, M. spicata exhibited, according to some studies, promising antioxidant, antidiabetic, anti-inflammatory, and anticancer effects, which show its potential to be used as a source for identifying natural drugs against cellular oxidative stress and its related diseases. Importantly, toxicological investigations of M. spicata show the safety of this species at different doses and several periods of use which justify its use in traditional medicines as tisane with tea. Here, we report, explore, and highlight the data published on M. spicata concerning its botanical description and geographical distribution, its phytochemical compounds, its pharmacological properties, and its toxicological investigations of M. spicata.

5.
Artículo en Inglés | MEDLINE | ID: mdl-35082904

RESUMEN

The purpose of this review is to summarize the available antidiabetic medicinal plants in the Kingdom of Saudi Arabia with its phytoconstituents and toxicological findings supporting by the latest literature. Required data about medicinal plants having antidiabetic activities and growing in the Kingdom of Saudi Arabia were searched/collected from the online databases including Wiley, Google, PubMed, Google Scholar, ScienceDirect, and Scopus. Keywords used in search are in vivo antidiabetic activities, flora of Saudi Arabia, active ingredients, toxicological evaluations, and medicinal plants. A total of 50 plant species belonging to 27 families were found in the flora of Saudi Arabia. Dominant family was found Lamiaceae with 5 species (highest) followed by Moraceae with 4 species. ß-Amyrin, ß-sitosterol, stigmasterol, oleanolic acid, ursolic acid, rutin, chlorogenic acid, quercetin, and kaempferol are the very common bioactive constituents of these selected plant species. This paper has presented a list of antidiabetic plants used in the treatment of diabetes mellitus. Bioactive antidiabetic phytoconstituents which showed that these plants have hypoglycemic effects and highly recommended for further pharmacological purposes and to isolate/identify antidiabetes mellitus (anti-DM) active agents also need to investigate the side effects of active ingredients.

6.
Drug Chem Toxicol ; 45(4): 1578-1586, 2022 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-33522322

RESUMEN

Diospyros kaki L.f. fruit and leaves are traditionally used for the treatment of hypertension, angina, internal hemorrhage, antithrombotic and anti-inflammatory effects.In the current study, the protective effects of ethyl acetate (Per-1), n-butanol (Per-2), and aqueous (Per-3) fractions of Diospyros kaki leaves against carbon tetrachloride (CCl4) induced nephrotoxicity in Swiss albino rats were tested. Animal were divided into nine groups; each group consists of six animals. The groups were : group I was untreated and kept as control, group II was treated with CCl4 only, group III (silymarin with CCl4); group IV (Per-1 100 mg/kg with CCl4);group V (Per-1 200 mg/kg with CCl4); group VI (Per-2 100 mg/kg with CCl4); group VII (Per-2 200 mg/kg with CCl4); group VIII (Per-3 100 mg/kg with CCl4); and group IX (Per-3 200 mg/kg with CCl4). Silymarin was used as standard drug. All tested fractions were found active (except Per-1 at low dose of 100 mg/kg) with significant value (p < 0.001) compared to CCl4 only group. Serum creatinine, malondialdehyde (MDA), and uric acid were significantly (p < 0.001) lowered in group VII-IX as compared to CCl4 only group. Similarly, total protein (TP) and non-protein sulfhydryls(NP-SH) level in kidney tissues were significantly (p < 0.001) elevated in the same groups compared to CCl4 only group. Further to check the cardio-protective potential, biochemical parameters such as LDH, creatine kinase, TP, MDA, and NP-SH levels in myocardial tissues were also estimated.These findings confirmed that the n-butanol and aqueous fractions are active and recommended for further bioactive phytoconstituents screening. Repeated column chromatography on silica gel G and sephadex-LH-20 of the active n-butanol fraction, four flavonoids were isolated. Based on the spectroscopic NMR data, compounds were identified as kaempferol (1), quercetin (2), astragalin (3), and rutin (4).


Asunto(s)
Diospyros , Silimarina , 1-Butanol/análisis , Animales , Antioxidantes/farmacología , Tetracloruro de Carbono/toxicidad , Diospyros/química , Frutas/química , Extractos Vegetales/química , Hojas de la Planta/química , Ratas , Suiza
7.
Artículo en Inglés | MEDLINE | ID: mdl-33510808

RESUMEN

Dodonaea viscosa is a medicinal plant which is being used to treat various diseases in humans. The available safety data suggest that the plant does not produce any side effects, or toxicity, in tested adult experimental animals. However, the influence of D. viscosa on fetus or embryonic development is largely not known. This study was conducted in order to find out the reproductive toxicity of D. viscosa in experimental animals. Zebrafish embryos were used as the in vivo developmental toxicity animal model. Methanolic crude extract, hexane, chloroform, and butanol fractions were prepared from the leaves of D. viscosa. Zebrafish embryos were exposed to serial dilution of crude extract and other fractions. The crude extract and hexane fraction induced higher level of toxicity in zebrafish embryos as compared to chloroform and butanol fractions. The phenol and flavonoid estimation revealed that crude leaves extract and hexane fractions had lower content of phenol and flavonoid. Two major compounds, phytol and methyl ester, of hexadecanoic acid were identified by gas chromatography and mass spectrophotometry (GC-MS) analysis. More detailed studies are needed to check the toxicity of D. viscosa in pregnant experimental animals; however, the results from this study have shown that D. viscosa possesses reproductive toxicity and its use and doses must be carefully monitored in pregnant patients.

8.
Nat Prod Res ; 35(12): 1959-1967, 2021 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-31364880

RESUMEN

Artemisia herba-alba is widely used in traditional medicines for the treatment of several diseases. From the aerial parts organic extract of A. herba-alba, two new compounds, 1,3,8-trihydroxyeudesm-4-en-7α,11ßH-12,6α-olide (1) and 5-ß-​D-​glucopyranosyloxy​-​7-methoxy-​6H-​benzopyran-​2-​one (2), respectively, together with five known metabolites: 3α,8ß-dihydroxygermacr-4(15),9(10)-dien-7ß,11αH,12,6α-olide (3), 1ß,8α-dihydroxy-11α,13-dihydrobalchanin (4), 11-epiartapshin (5), tomenin (6) and benzoic acid, p-​(ß-​D-​glucopyranosyloxy)​-​methyl ester (7), were isolated and identified. The chemical structures were proven depending upon spectroscopic analysis, including 1 D/2D NMR as and ESI-MS. Compound 1 inhibited Gram-positive bacteria Bacillus subtilis and Staphylococcus aureus. Compounds 2 and 3 exhibited antibacterial activity against both gram-positive and gram-negative bacteria.


Asunto(s)
Antibacterianos/química , Antibacterianos/farmacología , Artemisia/metabolismo , Artemisia/química , Bacillus subtilis/efectos de los fármacos , Evaluación Preclínica de Medicamentos , Bacterias Gramnegativas/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Estructura Molecular , Extractos Vegetales/química , Plantas Medicinales/química , Plantas Medicinales/metabolismo , Espectrometría de Masa por Ionización de Electrospray , Staphylococcus aureus/efectos de los fármacos
9.
Microsc Res Tech ; 84(1): 42-55, 2021 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-32852127

RESUMEN

In this study we have discussed pollen morphology of 14 mimosaceous species belonging to five genera by using light microscopy (LM) and scanning electron microscopy (SEM). The palynological features of species were determined by both qualitative and quantitative characters. The qualitative characters include pollen shape, colpi arrangement, and exine sculpturing. Oblate spheroidal shaped pollens were noted in Albizia procera, Albizia lebbeck, Acacia tortilis, Acacia ampliceps, and Acacia modesta, subprolate shaped pollen in Leucaena leucocephala, Prosopis julifera, and Acacia nilotica, prolate pollen in Acacia farnesiana and Prosopis glandulosa while spheroidal, sub spheroidal and sub oblate pollen grains were observed in Acacia catechu, Mimosa himalayana, Prosopis cineraria, respectively. Sparsely foveolate, reticulate, scabrate, and scrobiclate exine sculpturing were observed. Colpi with sunken ornamentation were seen in P. cineraria, P. glandulosa, P. juliflora, and L. leucocephala while colpi were absent in rest of the studied species. The quantitative characters were statistically studied using SPSS software. The current study gives important morpho-palynological characters for identifying and validation of close related and similar taxa which will aid to the phylogenetic analysis of Mimosaceae family.


Asunto(s)
Acacia , Fabaceae , Microscopía Electrónica de Rastreo , Filogenia , Polen , Especificidad de la Especie
10.
Artículo en Inglés | MEDLINE | ID: mdl-33343680

RESUMEN

BACKGROUND: Lichens present a complex symbiotic relationship between a filamentous fungus, photoautotrophic partner (algae or cyanobacteria), and bacterial community. The Objective of the Study. This study aimed at investigating the chemical composition and cytotoxic, antioxidant, and antimicrobial activities of acetone extracts of Moroccan Evernia prunastri (E. prunastri), Ramalina farinacea (R. farinacea), and Pseudevernia furfuracea (P. furfuracea). Materials and Methods. The phytochemical analysis was carried out by HPLC-UV. The cytotoxic effect was assessed on human prostate cancer (22RV1), human colon carcinoma (HT-29), human hepatocellular carcinoma (Hep-G2), and Hamster ovarian cancer (CHO) cells lines by WST1 assay. The antioxidant power was assessed by DPPH and FRAP assays. The antibacterial effect was obtained using the broth microdilution method. RESULTS: The findings of phytochemical analysis showed that the lichens studied possess interesting bioactive molecules such as physodalic acid, evernic acid, and usnic acid, as well as protocetraric acid. According to the American National Cancer Institute guidelines, the WST-1 test showed that all crude extracts did not show significant cytotoxic effects against all concerous cell lines, and IC50 values ranged from 42.30 to 140.24 µg/mL. Regarding the antioxidant activity, P. furfuracea extract showed the highest free-radical-scavenging ability (IC50 = 498.40 µg/mL). The most potent antibacterial extract was recorded for P. furfuracea extract with a minimum inhibitory concentration (MIC) ranging from 0.039 to 0.31 mg/mL. CONCLUSION: In this research work, we report that the studied lichen extracts exhibit an important biological effect, supporting that lichens represent a hopeful source of original natural products for the research of new bioactive molecules having a pharmaceutical interest.

11.
Molecules ; 25(21)2020 Oct 30.
Artículo en Inglés | MEDLINE | ID: mdl-33143247

RESUMEN

In this study, the aerial parts of Moricandia sinaica were evaluated for their in vivo analgesic, anti-inflammatory and antipyretic activities. The analgesic activities were examined using acetic acid-induced writhing, the hot plate test and the tail flick method. The anti-inflammatory and the antipyretic activities were evaluated using carrageenan-induced paw edema in rats and brewer's yeast-induced pyrexia in mice, respectively. The aqueous fraction of the methanol extract (MS-3) showed to be the most bioactive among the other investigated fractions. At the dose of 500 mg/kg, the fraction (MS-3) showed a significant percentage inhibition of the carrageenan-induced edema by 52.4% (p < 0.05). In addition, MS-3 exhibited a significant inhibition of acetic acid-induced writhes by 44.4% and 61.5% (p < 0.001) at 250-mg/kg and 500-mg/kg doses, respectively. At 120 min post-treatment, the rat groups treated with MS-3 displayed statistically significant reduction in rectal temperature (p < 0.001) by 1.7 °C and 2.2 °C at 250- and 500-mg/kg doses, respectively. The phytochemical composition of the fraction (MS-3) was characterized by high-performance liquid chromatography-mass spectrometry (HPLC-PDA-MS/MS). Molecular docking studies demonstrated that the polyphenols identified in MS-3 revealed good binding energy upon docking to some target proteins involved in pain response and inflammation, such as the cannabinoid receptors CB1 and CB2, the fatty acid amide hydrolase (FAAH) and the cyclooxygenase COX-1 and COX-2 enzymes. Based on the findings from the present work, it could be concluded that the aerial parts extract of M. sinaica exerts potential analgesic, anti-inflammatory and antipyretic effects in rats.


Asunto(s)
Analgésicos , Antiinflamatorios , Antipiréticos , Brassicaceae/química , Simulación del Acoplamiento Molecular , Extractos Vegetales/química , Polifenoles , Analgésicos/química , Analgésicos/farmacología , Animales , Antiinflamatorios/química , Antiinflamatorios/farmacología , Antipiréticos/química , Antipiréticos/farmacología , Polifenoles/química , Polifenoles/farmacología , Ratas , Ratas Wistar
12.
Mol Biol Rep ; 47(8): 6043-6051, 2020 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-32700127

RESUMEN

Centaurea bruguierana, of the Asteraceae family, has a long history of use in traditional medicines for the treatment of various ailments. However, the anticancer activity and underlying mechanisms have not yet been assessed. The C. bruguierana was extracted with methanol and fractionated into four different fractions. Different cancer cells and one non-cancerous were used to examine the cytotoxic effects of these fractions using MTT assay. The most potent fraction, C. bruguierana ethyl acetate fraction (CB EtOAc), was explored for its effects on cell cycle progression and apoptosis induction by Hoechst staining and annexin V-PI double staining in MCF-7 cells. The expression of apoptosis-related genes was quantified by RT-PCR. Of all fractions, CB EtOAc was found to have the strongest antiproliferative activity (IC50 = 10 µg/mL) against MCF-7 cells. The antiproliferative activity of the CB EtOAc fraction against MCF-7 was correlated with arrested of cell cycle in the G1 phase, nuclear fragmentation, and the exposure of phosphatidylserine. The induction of apoptosis by CB EtOAc in MCF-7 cells was also associated with an increase in the Bax/Bcl-2 ratio and higher expression of caspases. Overall, our results demonstrated that CB EtOAc showed apoptosis-inducing effects, suggesting that C. bruguierana may be a promising source for a novel chemotherapeutic agents for the treatment of breast cancer.


Asunto(s)
Antineoplásicos Fitogénicos/aislamiento & purificación , Neoplasias de la Mama/patología , Centaurea/química , Extractos Vegetales/farmacología , 1-Butanol , Células A549 , Acetatos , Animales , Antineoplásicos Fitogénicos/farmacología , Apoptosis/efectos de los fármacos , Proteínas Reguladoras de la Apoptosis/biosíntesis , Proteínas Reguladoras de la Apoptosis/genética , Puntos de Control del Ciclo Celular/efectos de los fármacos , División Celular/efectos de los fármacos , Núcleo Celular/efectos de los fármacos , Núcleo Celular/ultraestructura , Cloroformo , Ensayos de Selección de Medicamentos Antitumorales , Femenino , Regulación Neoplásica de la Expresión Génica/efectos de los fármacos , Células Hep G2 , Células Endoteliales de la Vena Umbilical Humana , Humanos , Concentración 50 Inhibidora , Células MCF-7 , Metanol , Proteínas de Neoplasias/biosíntesis , Proteínas de Neoplasias/genética , Componentes Aéreos de las Plantas/química , Solventes
13.
Molecules ; 25(9)2020 May 06.
Artículo en Inglés | MEDLINE | ID: mdl-32384789

RESUMEN

Genus Stachys, the largest genera of the family Lamiaceae, and its species are frequently used as herbal teas due to their essential oils. Tubers of some Stachys species are also consumed as important nutrients for humans and animals due to their carbohydrate contents. Three new neo-clerodane diterpene peroxides, named stachaegyptin F-H (1, 2, and 4), together with two known compounds, stachysperoxide (3) and stachaegyptin A (5), were isolated from Stachys aegyptiaca aerial parts. Their structures were determined using a combination of spectroscopic techniques, including HR-FAB-MS and extensive 1D and 2D NMR (1H, 13C NMR, DEPT, 1H-1H COSY, HMQC, HMBC and NOESY) analyses. Additionally, a biosynthetic pathway for the isolated compounds (1-5) was discussed. The chemotaxonomic significance of the isolated diterpenoids of S. aegyptiaca in comparison to the previous reported ones from other Stachys species was also studied.


Asunto(s)
Diterpenos de Tipo Clerodano/análisis , Fitoquímicos/análisis , Componentes Aéreos de las Plantas/química , Extractos Vegetales/análisis , Stachys/química , Vías Biosintéticas , Clasificación , Diterpenos/análisis , Diterpenos/aislamiento & purificación , Diterpenos de Tipo Clerodano/química , Diterpenos de Tipo Clerodano/aislamiento & purificación , Espectroscopía de Resonancia Magnética , Modelos Moleculares , Estructura Molecular , Peróxidos/análisis , Peróxidos/aislamiento & purificación , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación , Extractos Vegetales/química , Tés de Hierbas/análisis
14.
Drug Des Devel Ther ; 13: 4195-4205, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31849451

RESUMEN

BACKGROUND: Cancer is one of the chronic health conditions worldwide. Various therapeutically active compounds from medicinal plants were the current focus of this research in order to uncover a treatment regimen for cancer. Anchusa arvensis (A. anchusa) (L.) M.Bieb. contains many biologically active compounds. METHODS: In the current study, new ester 3-hydroxyoctyl -5- trans-docosenoate (compound-1) was isolated from the chloroform soluble fraction of A. anchusa using column chromatography. Using MTT assay, the anticancer effect of the compound was determined in human hepatocellular carcinoma cells (HepG-2) compared with normal epithelial cell line (Vero). DPPH and ABTS radical scavenging assays were performed to assess the antioxidant potential. The Molecular Operating Environment (MOE-2016) tool was used against tyrosine kinase. RESULTS: The structure of the compound was elucidated based on IR, EI, and NMR spectroscopy technique. It exhibited a considerable cytotoxic effect against HepG-2 cell lines with IC50 value of 6.50 ± 0.70 µg/mL in comparison to positive control (doxorubicin) which showed IC50 value of 1.3±0.21 µg/mL. The compound did not show a cytotoxic effect against normal epithelial cell line (Vero). The compound also exhibited significant DPHH scavenging ability with IC50 value of 12 ± 0.80 µg/mL, whereas ascorbic acid, used as positive control, demonstrated activity with IC50 = 05 ± 0.15 µg/mL. Similarly, it showed ABTS radical scavenging ability (IC50 = 130 ± 0.20 µg/mL) compared with the value obtained for ascorbic acid (06 ± 0.85 µg/mL). In docking studies using MOE-2016 tool, it was observed that compound-1 was highly bound to tyrosine kinase by having two hydrogen bonds at the hinge region. This good bonding network by the compound might be one of the reasons for showing significant activity against this enzyme. CONCLUSION: Our findings led to the isolation of a new compound from A. anchusa which has significant cytotoxic activity against HepG-2 cell lines with marked antioxidant potential.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Benzotiazoles/antagonistas & inhibidores , Compuestos de Bifenilo/antagonistas & inhibidores , Boraginaceae/química , Ésteres/farmacología , Ácidos Grasos Monoinsaturados/farmacología , Picratos/antagonistas & inhibidores , Ácidos Sulfónicos/antagonistas & inhibidores , Animales , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Proliferación Celular/efectos de los fármacos , Chlorocebus aethiops , Simulación por Computador , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Ésteres/química , Ésteres/aislamiento & purificación , Ácidos Grasos Monoinsaturados/química , Ácidos Grasos Monoinsaturados/aislamiento & purificación , Células Hep G2 , Humanos , Simulación del Acoplamiento Molecular , Estructura Molecular , Plantas Medicinales , Relación Estructura-Actividad , Células Vero
15.
Drug Des Devel Ther ; 13: 3029-3036, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31692531

RESUMEN

BACKGROUND: Traditionally, Grewia optiva is widely used for the treatment of many diseases like dysentery, fever, typhoid, diarrhea, eczema, smallpox, malaria and cough. METHODS: Shade-dried roots of G. optiva were extracted with methanol. Based on HPLC results, chloroform and ethyl acetate fractions were subjected to silica column isolation and four compounds: glutaric acid (V), 3,5 dihydroxy phenyl acrylic acid (VI), (2,5 dihydroxy phenyl) 3',6',8'-trihydroxyl-4H chromen-4'-one (VII) and hexanedioic acid (VIII) were isolated in pure form. Ellman's assay was used to determine the anticholinesterase potential of isolated compounds while their antioxidant potential was estimated by DPPH and ABTS scavenging assays. RESULTS: Amongst the isolated compounds, VI and VII exhibited excellent percent inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) (83.23±1.11, 82.72±2.20 and 82.11±2.11, 82.23±1.21, respectively, at 1000 µg/mL) with IC50 of 76, 90, 78 and 92 µg/mL, respectively. Highest percent radicals scavenging against DPPH and ABTS (87.41±1.20 and 86.13±2.31) with IC50 of 64 and 65 µg/mL, respectively, were observed for compound VII. Molecular docking studies also supported the binding of compound VI and VII with the target enzyme. The para-hydroxyl group of the phenolic moiety is formed hydrogen bonds with the active site water molecule and the side chain carbonyl and hydroxyl residues of enzyme. CONCLUSION: The isolated compounds inhibited the DPPH and ABTS-free radicals, and AChE and BChE enzymes. It was concluded that these compounds could be used in relieving the oxidative stress and pathological symptoms associated with excessive hydrolysis of acetyl and butyryl choline. The results of the study were supported by docking studies for compounds VI and VII.


Asunto(s)
Antioxidantes/farmacología , Inhibidores de la Colinesterasa/farmacología , Grewia/química , Extractos Vegetales/farmacología , Acetilcolinesterasa/efectos de los fármacos , Acetilcolinesterasa/metabolismo , Antioxidantes/administración & dosificación , Butirilcolinesterasa/efectos de los fármacos , Butirilcolinesterasa/metabolismo , Inhibidores de la Colinesterasa/administración & dosificación , Depuradores de Radicales Libres/farmacología , Concentración 50 Inhibidora , Simulación del Acoplamiento Molecular , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/administración & dosificación , Raíces de Plantas
16.
Nutrients ; 11(10)2019 Oct 07.
Artículo en Inglés | MEDLINE | ID: mdl-31591364

RESUMEN

BACKGROUND: Plants belonging to the genus Kaempferia (family: Zingiberaceae) are distributed in Asia, especially in the southeast region, and Thailand. They have been widely used in traditional medicines to cure metabolic disorders, inflammation, urinary tract infections, fevers, coughs, hypertension, erectile dysfunction, abdominal and gastrointestinal ailments, asthma, wounds, rheumatism, epilepsy, and skin diseases. OBJECTIVE: Herein, we reported a comprehensive review, including the traditional applications, biological and pharmacological advances, and phytochemical constituents of Kaempheria species from 1972 up to early 2019. MATERIALS AND METHODS: All the information and reported studies concerning Kaempheria plants were summarized from library and digital databases (e.g., Google Scholar, Sci-finder, PubMed, Springer, Elsevier, MDPI, Web of Science, etc.). The correlation between the Kaempheria species was evaluated via principal component analysis (PCA) and agglomerative hierarchical clustering (AHC), based on the main chemical classes of compounds. RESULTS: Approximately 141 chemical constituents have been isolated and reported from Kaempferia species, such as isopimarane, abietane, labdane and clerodane diterpenoids, flavonoids, phenolic acids, phenyl-heptanoids, curcuminoids, tetrahydropyrano-phenolic, and steroids. A probable biosynthesis pathway for the isopimaradiene skeleton is illustrated. In addition, 15 main documented components of volatile oils of Kaempheria were summarized. Biological activities including anticancer, anti-inflammatory, antimicrobial, anticholinesterase, antioxidant, anti-obesity-induced dermatopathy, wound healing, neuroprotective, anti-allergenic, and anti-nociceptive were demonstrated. CONCLUSIONS: Up to date, significant advances in phytochemical and pharmacological studies of different Kaempheria species have been witnessed. So, the traditional uses of these plants have been clarified via modern in vitro and in vivo biological studies. In addition, these traditional uses and reported biological results could be correlated via the chemical characterization of these plants. All these data will support the biologists in the elucidation of the biological mechanisms of these plants.


Asunto(s)
Fitoquímicos/uso terapéutico , Fitoterapia , Extractos Vegetales/uso terapéutico , Zingiberaceae/química , Animales , Humanos , Fitoquímicos/efectos adversos , Fitoquímicos/aislamiento & purificación , Extractos Vegetales/efectos adversos , Extractos Vegetales/aislamiento & purificación , Zingiberaceae/clasificación
17.
Biomed Res Int ; 2019: 2403718, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31317024

RESUMEN

This study investigated the phytochemical characteristics and antioxidant activity in leaves, roots, stem, flower, and seed parts of Datura alba (D. alba). The study also assessed the heavy metal (Cr, Mn, Zn, and Cu) accumulation in each part of the plant. Among the phytochemicals, alkaloids were found only in leaves while tannins, flavonoids, and phenols were present in all parts of the plant. For antioxidant activity, free radical scavenging assay for 2,2-diphenyl-1-picrylhydrazyl (DPPH) was performed using ascorbic acid as the standard. Higher activity was shown by stem extract in methanol and leaf extract in n-hexane, ethyl acetate, and chloroform. Furthermore, all the target heavy metals were detected in all plant sections with the highest concentration of Zn in leaves and Cu in stem, root, flower, and seed. Due to stronger antioxidant potential and phytochemical composition, D. alba could prove as valuable prospect in pharmaceutical formulations by taking part in the antioxidant defense system against generation of free radicals.


Asunto(s)
Antioxidantes/química , Datura/química , Radicales Libres/antagonistas & inhibidores , Metales Pesados/aislamiento & purificación , Fitoquímicos/aislamiento & purificación , Alcaloides/química , Alcaloides/aislamiento & purificación , Antioxidantes/farmacología , Flavonoides/química , Flavonoides/aislamiento & purificación , Metales Pesados/química , Metales Pesados/clasificación , Fenoles/química , Fenoles/aislamiento & purificación , Fitoquímicos/química , Fitoquímicos/clasificación , Extractos Vegetales/química , Extractos Vegetales/farmacología , Hojas de la Planta/química , Semillas/química , Taninos/química , Taninos/clasificación , Taninos/aislamiento & purificación
18.
J Food Drug Anal ; 27(3): 758-765, 2019 07.
Artículo en Inglés | MEDLINE | ID: mdl-31324291

RESUMEN

In traditional Arabian medicine, the Rhus tripartita plant (family Anacardiaceae) has been used to treat inflammatory conditions. Although Rhus extracts have been reported for their cardioprotective effects, information regarding their active principle compounds remains insufficient. The present investigation was aimed at determining the antioxidant chemical constituents of the methanolic extract of R. tripartita stem bark and evaluating their ability to ameliorate methylglyoxal-induced endothelial cell apoptosis. Ten flavonoid compounds (1-10) were isolated and identified using DPPH radical scavenging bioassay-guided chromatographic separation. A new proanthocyanidin (rhuspartin) (1) was isolated and identified as 3,5,13,14-flavantetrol-(4ß→8)-catechin, using extensive spectroscopic data and high resolution-mass spectrometry. Among the compounds (1, 5, 7-10) tested for toxicity toward cultured endothelial cells (HUVECs), the non-cytotoxic compounds 1 and 7 evinced cytoprotective potential that reversed the methylglyoxal-induced apoptosis (by 62% and 64%, respectively) through downregulation of caspase 3/7.


Asunto(s)
Antioxidantes/farmacología , Apoptosis/efectos de los fármacos , Células Endoteliales de la Vena Umbilical Humana/efectos de los fármacos , Extractos Vegetales/farmacología , Proantocianidinas/farmacología , Rhus/química , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Compuestos de Bifenilo/antagonistas & inhibidores , Proliferación Celular/efectos de los fármacos , Humanos , Cetonas/antagonistas & inhibidores , Cetonas/farmacología , Picratos/antagonistas & inhibidores , Corteza de la Planta/química , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Tallos de la Planta/química , Proantocianidinas/química , Proantocianidinas/aislamiento & purificación
19.
Artículo en Inglés | MEDLINE | ID: mdl-31354848

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Aristolochia paucinervis (A. paucinervis) (Aristolochiaceae) is a plant frequently used in Moroccan alternative medicine. The aim of the current study is to investigate the phytochemical composition of rhizomes decoction of A. paucinervis (RDA) and to evaluate its acute and subacute toxicity following the OECD guidelines. MATERIALS AND METHODS: The qualitative phytochemical analysis of A. paucinervis was performed using standard qualitative phytochemical procedures. The acute toxicity of rhizomes decoction of the studied plant was evaluated in mice at single doses of 1, 2, and 4 g/kg of body weight for 14 days. In subacute toxicity study, the decoction was orally administered to mice at three different doses (0.5, 1, and 1.5 g/kg/day) for 28 days. Histopathological and biochemical parameters were investigated. RESULTS: The preliminary phytochemical screening showed the presence of flavonoids, saponins, alkaloids, and polyphenols and the absence of anthraquinones, sterols, and terpenes. There was no mortality and no significant changes occurred in animals treated with 1 and 2 g/kg in the acute toxicity model. The signs of toxicity and morbidity were remarkable with the highest tested dose (4g/kg). LD50 (dose required to kill 50% of the test population) was determined as 4 g/kg. Repeated oral administration of 1 and 1.5 g/kg/day of RDA for 28 days induced significant disturbance of serum parameters (AST, ALT, LDH, urea, creatinine). Kidney and liver extracted from mice fed with 1 and 1.5 g/kg/day showed significant histopathological injuries as tubular necrosis, inflammatory infiltrate, tubular degeneration, necrosis, and hepatic cholestasis. Meanwhile, neither histopathological nor biochemical alterations were observed in mice treated with 0.5 g/kg/day of body weight in comparison to the control group. CONCLUSION: RDA showed toxicity in mice at a dose of 1 g/kg/day under subacute toxicity conditions. RDA is safe at a single dose inferior to 4 g/kg of body weight. The plant extract prepared by decoction showed more poisonous effect than the extract prepared by maceration at room temperature.

20.
Molecules ; 24(13)2019 Jun 29.
Artículo en Inglés | MEDLINE | ID: mdl-31261927

RESUMEN

Euphorbia species were widely used in traditional medicines for the treatment of several diseases. From the aerial parts of Egyptian endemic plant, Euphorbia sanctae-catharinae, three new premyrsinane diterpenoids, namely, euphosantianane E-G (1-3), alongside four known triterpenes, 9,19-cyclolanostane-3ß,24S-diol (4), 25-methoxycycloartane-3ß,24S-diol (5), 25-methylenecycloartan-3ß,24R-diol (6), and 25-methylenecycloartan-3ß,24S-diol (7), were isolated and identified. The chemical structures were proven depending upon spectroscopic analysis, including FTIR, HRFABMS, and 1D/2D-NMR. The chemotaxonomic significance of the isolated compounds, especially diterpenes from E. sanctae-catharinae compared to those documented from different Euphorbia species was also studied via agglomerative hierarchical clustering (AHC). The Egyptian endemic Euphorbia sanctae-catharina was grouped with E. bupleuroides, E. fidjiana, E. fischeriana, E. pithyusa subsp. cupanii, E. prolifera, and E. seguieriana, where myrsinol diterpenoids were the characteristic compounds.


Asunto(s)
Antineoplásicos Fitogénicos/síntesis química , Diterpenos/síntesis química , Euphorbia/química , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Diterpenos/química , Diterpenos/farmacología , Ensayos de Selección de Medicamentos Antitumorales , Egipto , Estructura Molecular , Componentes Aéreos de las Plantas/química , Extractos Vegetales/química
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